Process of preparing tablets



Patented Feb. 2 7, 1940 I 7 2191.678 PROCESS OF PREPARING TABLETSFerdinand W. Nitardy, Brooklyn, and Lionel T. Andrews, Jamaica, N. Y.,assignors to E. R. Squibb & Sons, New York, N. Y., a corporation of NewYork No Drawing. Application April 2, 1938,

Serial No. 199,736

8 Claims.

This invention relates to the production of tablets by compression.

Difilculties are encountered in compressing certain tablet granulationson account of the tendency of the granulation to adhere to the punchesand dies, resulting in malformation of the tablet and/or jamming of themachinery. Attempts have been made to obviate these difficulties by theuse of lubricants for the compression; lycopodium powder, talcum powder,and liquid petrolatum, inter alia, being frequently used for thispurpose. However, the lubricants heretofore employed have not beencompletely satisfactory, either being required in excessive amounts, or,as in the case of granulations embodying hygroscopic ingredients (suchas ammonium mandelate and sodium salicylate) being partially or whollyineffective.

It is the object of this invention to provide effective and economicallubricants for the production of tablets by compression, particularlytablets embodying hygroscopic ingredients.

It has been found that water-insoluble soaps, especially magnesiumstearate, are suitable lubricants for the production of tablets bycompression, being eifective in much smaller proportions (e. g. as lowas about 0.1% of the weight of the tablet) than those of the lubricantsheretofore employed and enabling the production of tablets fromgranulations embodying hygroscopic ingredients (such as ammoniummandelate) which could not heretofore be made by compression.

The effective soaps comprise, inter alia, the magnesium, calcium, zinc,aluminum, lithium, bismuth, copper, iron, and manganese salts of higherfatty acids or mixtures such as stearic,

. palmitic, lauric, myristic, and cocoanut-oil fatty acids. In additionto their lubricating property,

these soaps have water-repellent properties, and. it is apparently thiscombination of properties that enables the production of tablets bycompression from granulations embodying hygroscopic ingredients such asammonium mandelate. Manifestly, the particular soap employed should beinert to, or compatible with, the other ingredients of the tablet, and,in the case of pharmaceuticals, should also be innocuous.

Preferably, the soap is incorporated into the granulation by dusting itin finely divided form over the granulation prior to compression, thuscovering the granules with a thin layer of the soap. Granulationsembodying a water-insoluble soap as a lubricant are readily compressedand ejected from the die; moveover, the use of these lubricants resultsin an increase in speed of tableting, since operations need not bestopped for cleaning of the punches and dies.

The following examples are illustrative of the invention:

Example 1 Ingredients for making one thousand 7 /2- grain ammoniummandelate tablets:

Ammonium mandelate g 486 Magnesium stearate g 19.5

486 g. lumpy ammonium mandelate is granulated and thoroughly admixedwith part of the magnesium stearate; the mixture is regranulated,compressed into small slugs, again granulated, thoroughly admixed withthe remainder of the magnesium stearate, regranulated, and compressedinto tablets. The compression" is readily effected, the tablets beingeasily and cleanly ejected. Theresulting tablets are, moreover,relatively stable in the atmosphere.

The ingredients named in the following examples are mixed and granulatedin the usual manner, the water-insoluble soap is dusted over the drygranulation, and the granulation compressed into tablets. Compressionand ejection are readily effected without encountering any sticking tothe punches and dies, and the resulting tablets are hard, smooth, andunbroken.

ner.

Example 3 Ingredients for making 10,000 fi-grain yeast tablets:

Brewers yeast kg 3.24

Malted-wheat-germextract kg 1.59

Sucrose kg 1.235

Citric acid g 61 Magnesium stearate -g 7.5

Example 4 Ingredients for making 2,750 5-grain sodium salicylatetablets:

Sodium salicylate g 891 Sucrose g 137 Acacia g 38.5 Lactose g 20Magnesium stearate g- 20 Example 5 Ingredients for making 1,000 2.5-gramsodium hydroxide tablets:

Sodium hydroxide (granular) kg 2.500 Aluminum stearate g 100 Thelubricants of this invention may be substituted generally for theheretofore employed lubricants. In addition to those detailed in theforegoing examples, the following tablets, inter alia, may be readilyprepared when using the lubricants of this invention:

Cascara sagrada Quinine sulfate Aloe and mastic (NF VI).

Aloin. strychnine, and belladonna (NF VI) Asafetida NF VI) Camphor,quinine sulfate, and belladonna Sodium glycerophosphate and calciumglycerophosphate 3. The process of preparing tablets which comprisesdusting a tablet granulation with a lubricant consisting of awater-insoluble soap, and compressing the granulation into tablets.

4. The process of preparing tablets which comprises dusting a tabletgranulation with a lubricant consisting of magnesium stearate, andcompressing the granulation into tablets.

5. In the process of preparing tabletsby compressing a granulationembodying a hygroscopic ingredient, the step of incorporating in thegranulation a lubricant consisting of a water-insoluble soap.

6. The process of preparing ammonium mandelate tablets which comprisesdusting a granulation of ammonium mandelate with a lubricant consistingof a water-insoluble soap, and compressing the granulation into tablets.

'7. The process of preparing sodium salicylate tablets which comprisesdusting a granulation essentially comprising sodium salicylate with alubricant consisting of a water-insoluble soap, and compressing thegranulation into tablets.

8. The process of preparing sodium hydroxide tablets which comprisesdusting a granulation of sodium hydroxide with a lubricant consisting ofa water-insoluble soap, and compressing the granulation into tablets.

FERDINAND W. NITARDY. LIONEL T. ANDREWS.

